Discovery and synthesis of [6-hydroxy-3-[4-[2-(1-piperidinyl) ethoxy] phenoxy]-2-(4-hydroxyphenyl)] benzo [b] thiophene: a novel, highly potent, selective estrogen …

AD Palkowitz, AL Glasebrook, KJ Thrasher…

文献索引：Palkowitz, Alan D.; Glasebrook, Andrew L.; Thrasher, K. Jeff; Hauser, Kenneth L.; Short, Lorri L.; Phillips, D. Lynn; Muehl, Brian S.; Sato, Masahiko; Shetler, Pamela K.; Cullinan, George J.; Pell, Tina R.; Bryant, Henry U. Journal of Medicinal Chemistry, 1997 , vol. 40, # 10 p. 1407 - 1417

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被引用次数: 185

摘要

Raloxifene,[2-(4-hydroxyphenyl)-6-hydroxybenzo [b] thien-3-yl][4-[2-(1-piperidinyl) ethoxy] phenyl] methanone hydrochloride (2), is representative of a class of compounds known as selective estrogen receptor modulators (SERMs) that possess estrogen agonist-like actions on bone tissues and serum lipids while displaying potent estrogen antagonist properties in the breast and uterus. As part of ongoing SAR studies with raloxifene, we found that ...